Study of the ^99mTc‐labeling conditions of 6‐hydrazinonicotinamide‐conjugated peptides from a new perspective: Introduction to the term radio‐stoichiometry

Abstract

Specific tumor uptake of peptide radiopharmaceuticals depends on tumor binding affinity and their radiochemical purity. Several important parameters that influence the 99mTc‐labeling and consequently the radiochemical purity of 6‐hydrazinonicotinamide (HYNIC)‐conjugated peptide are radionuclide activity, the amount of peptide, the amount of coligands, and the amount of reducing agents (stannous ion). In this review article, we have attempted studying these parameters in the HYNIC‐conjugated peptides (somatostatin, cholecystokinin/gastrin, bombesin, and RGD analogs) from a new perspective to obtain most used and optimized radio‐stoichiometric relationships. One of the most important results in this review is that for 99mTc‐labeling of HYNIC‐conjugated peptides, it is better to consider the most calculated mole ratio between technetium‐99m and the peptide (mole ratio of technetium‐99m to the peptide 1:200–400). The statistical results also show that among these 99mTc‐labeled peptides, the most used and favorable coligand is tricine/EDDA with two to one (2:1) mole ratio. These optimized radio‐stoichiometric relationships, favorable coligand mole ratio, and applicable radiolabeling points can greatly improve the labeling process of the HYNIC‐conjugated peptides, by reducing trial and error, increasing specific activity, and saving materials.